Assay Detail
Binding
CHEMBL3991817
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
242
Total Activities
242
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K-562, COLO 205, SK-N-BE(2) and MV-4-11 |
| Subcellular | Cell lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 6.16 | 8.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.40 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.40 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.72 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.51 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.46 |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | 7.04 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.00 |
| CHEMBL3688339 | — | — | 1 | 6.99 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.97 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | 6.96 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.69 |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | 6.56 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.54 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 6.54 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 6.50 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.39 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.37 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.36 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.29 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.29 |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | 6.26 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.26 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 6.26 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 6.20 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 6.13 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.04 |
| CHEMBL281948 | K-252A | — | 1 | 6.00 |
| CHEMBL3699142 | — | — | 1 | 5.96 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.95 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL1721885 | SU-014813 | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL522892 | DOVITINIB | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL2180604 | TAK-593 | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL3688339 | — | Kd | = | 103.0 | nM | 6.99 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL403989 | TG100-801 | Kd | = | 109.0 | nM | 6.96 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 203.0 | nM | 6.69 |
| CHEMBL2220486 | LUCITANIB | Kd | = | 278.0 | nM | 6.56 |
| CHEMBL5416410 | DASATINIB | Kd | = | 292.0 | nM | 6.54 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 288.0 | nM | 6.54 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 316.0 | nM | 6.50 |
| CHEMBL1289926 | AXITINIB | Kd | = | 404.0 | nM | 6.39 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL574737 | UCN-01 | Kd | = | 436.0 | nM | 6.36 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 510.0 | nM | 6.29 |
| CHEMBL564829 | MILCICLIB | Kd | = | 512.0 | nM | 6.29 |
| CHEMBL1822792 | MK-2461 | Kd | = | 543.0 | nM | 6.26 |
| CHEMBL2079588 | TELATINIB | Kd | = | 555.0 | nM | 6.26 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 552.0 | nM | 6.26 |
| CHEMBL217092 | SARACATINIB | Kd | = | 631.0 | nM | 6.20 |
| CHEMBL274654 | ORANTINIB | Kd | = | 744.0 | nM | 6.13 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 907.0 | nM | 6.04 |
| CHEMBL281948 | K-252A | Kd | = | 1006.0 | nM | 6.00 |
| CHEMBL3699142 | — | Kd | = | 1107.0 | nM | 5.96 |
| CHEMBL3545328 | XL-019 | Kd | = | 1118.0 | nM | 5.95 |
| CHEMBL253969 | OSI-632 | Kd | = | 1146.0 | nM | 5.94 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 1364.0 | nM | 5.87 |
| CHEMBL223360 | LINIFANIB | Kd | = | 1551.0 | nM | 5.81 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 1607.0 | nM | 5.79 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1735.0 | nM | 5.76 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1795.0 | nM | 5.75 |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | = | 1892.0 | nM | 5.72 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 2409.0 | nM | 5.62 |
| CHEMBL377300 | BRIVANIB | Kd | = | 2537.0 | nM | 5.60 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 2550.0 | nM | 5.59 |
| CHEMBL415049 | BARASERTIB | Kd | = | 2692.0 | nM | 5.57 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 2666.0 | nM | 5.57 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 2776.0 | nM | 5.56 |
| CHEMBL206834 | BAFETINIB | Kd | = | 3132.0 | nM | 5.50 |
| CHEMBL1171837 | PONATINIB | Kd | = | 3285.0 | nM | 5.48 |
| CHEMBL3991933 | — | Kd | = | 3609.0 | nM | 5.44 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 3988.0 | nM | 5.40 |
| CHEMBL101253 | VATALANIB | Kd | = | 4393.0 | nM | 5.36 |
| CHEMBL3544932 | TAK-901 | Kd | = | 4592.0 | nM | 5.34 |
| CHEMBL1908391 | MASITINIB | Kd | = | 4743.0 | nM | 5.32 |
| CHEMBL587723 | AEE-788 | Kd | = | 9383.0 | nM | 5.03 |